Omipalisib (GSK2126458) | PI3K/mTOR inhibitor

Chemical Structure : Omipalisib

CAS No.: 1086062-66-9

Omipalisib (GSK458, GSK-2126458, GSK2126458)

Catalog No.: PC-42513Not For Human Use, Lab Use Only.

Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.

Packing	Price	Stock
10 mg	$78	In stock
25 mg	$128	In stock
50 mg	$218	In stock
100 mg	$358	In stock
250 mg		Get quote

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Biological Activity

Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.
GSK2126458 shows equivalent activity for p110α mutants E542K/E545K/H1047R with Ki of 8/8/9 nM.
GSK2126458 inhibits pAKT-S473 in T47D cells (IC50=0.41 nM), also inhibits phosphorylation of AKTT308 and p70S6K.
GSK2126458 is active in vivo and orally bioavailable.

Physicochemical Properties

M.Wt	505.496
Formula	C25H17F2N5O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-

References

1. Knight SD, et al. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43.

2. Khalili JS, et al. Clin Cancer Res. 2012 Aug 15;18(16):4345-55.

3. Munster P, et al. Clin Cancer Res. 2016 Apr 15;22(8):1932-9.

Omipalisib (GSK458, GSK-2126458, GSK2126458)

Biological Activity

Physicochemical Properties

References

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